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GW4064 is an agonist of FXR with EC50 values of 15nM and 90nM, respectively in an isolated receptor activity assay and in cells transfected with human FXR [1].

GW4064 is identified as a highly effective, selective, nonsteroidal agonist of FXR. It shows beneficial effects on cholesterol and TG in various animal species. GW4064 is found to lower serum TG levels in both the KK-Ay and ob/ob mice potently. In KK-Ay mice, a 1-week administration of GW4064 also significantly lowers VLDL secretion. And in the SHP+/+ mice, GW4064 can also lower serum TGs. [2]

Due to some limitations, such as limited solubility, potentially toxic stilbene pharmacophore and UV light instability, GW4064 is not a good candidate of drug. It is now usually used as a tool compound for investigating the physiological functions of FXR [3].

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